Zirconium tetraazamacrocycle complexes display extraordinary stability and provide a new strategy for zirconium-89-based radiopharmaceutical development

Darpan N Pandya; Nikunj Bhatt; Hong Yuan; Cynthia S Day; Brandie M Ehrmann; Marcus Wright; Ulrich Bierbach; Thaddeus J Wadas

doi:10.1039/c6sc04128k

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Zirconium tetraazamacrocycle complexes display extraordinary stability and provide a new strategy for zirconium-89-based radiopharmaceutical development

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Zirconium tetraazamacrocycle complexes display extraordinary stability and provide a new strategy for zirconium-89-based radiopharmaceutical development

Darpan N Pandya, Nikunj Bhatt, Hong Yuan, Cynthia S Day, Brandie M Ehrmann, Marcus Wright, Ulrich Bierbach and Thaddeus J Wadas

Chemical science (Cambridge), Vol.8(3), pp.2309-2314

03/01/2017

DOI: 10.1039/c6sc04128k

PMCID: PMC5363373

PMID: 28451334

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Abstract

We report our initial investigations into the use of tetraazamacrocycles as zirconium-89 chelators. We describe the synthesis and complete characterization of several Zr tetraazamacrocycle complexes, and definitively describe the first crystal structure of zirconium 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (Zr-DOTA) using single crystal X-ray diffraction analysis. After evaluating several radioactive analogs, we found that Zr-DOTA is superior to Zr-DFO, the only Zr-complex to be used clinically in Zr-radiopharmaceutical applications. Finally, we provide a rationale for the unanticipated and extraordinary stability of these complexes and . These results may inform the development of safer and more robust immuno-PET agents for precision medicine applications.

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Title: Subtitle: Zirconium tetraazamacrocycle complexes display extraordinary stability and provide a new strategy for zirconium-89-based radiopharmaceutical development
Creators: Darpan N Pandya - Wake Forest University
Nikunj Bhatt - Wake Forest University
Hong Yuan - University of North Carolina at Chapel Hill
Cynthia S Day - Wake Forest University
Brandie M Ehrmann - University of North Carolina at Chapel Hill
Marcus Wright - Wake Forest University
Ulrich Bierbach - Wake Forest University
Thaddeus J Wadas - Wake Forest University
Resource Type: Journal article
Publication Details: Chemical science (Cambridge), Vol.8(3), pp.2309-2314
DOI: 10.1039/c6sc04128k
PMID: 28451334
PMCID: PMC5363373
NLM abbreviation: Chem Sci
ISSN: 2041-6520
eISSN: 2041-6539
Grant note: P30 CA016086 / NCI NIH HHS UL1 TR001420 / NCATS NIH HHS
Language: English
Date published: 03/01/2017
Academic Unit: Radiology; Radiation Oncology
Record Identifier: 9984313076302771

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